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1型光疗剂,第一部分:新型光不稳定亚磺酰胺的制备及癌细胞活力研究

Type 1 phototherapeutic agents, part I: preparation and cancer cell viability studies of novel photolabile sulfenamides.

作者信息

Karwa Amolkumar S, Poreddy Amruta R, Asmelash Bethel, Lin Tien-Sung, Dorshow Richard B, Rajagopalan Raghavan

机构信息

Covidien Pharmaceuticals , 675 McDonnell Boulevard, Hazelwood, Missouri 63042, United States.

Department of Chemistry, Washington University , 1 Brookings Drive, St. Louis, Missouri 63130, United States.

出版信息

ACS Med Chem Lett. 2011 Sep 13;2(11):828-33. doi: 10.1021/ml2001483. eCollection 2011 Nov 10.

Abstract

Novel type 1 phototherapeutic agents based on compounds containing S-N bonds (sulfenamides) were synthesized, assessed for free radical generation, and evaluated in vitro for cell death efficacy in four cancer cell lines (U937, HTC11, KB, and HT29). All of the compounds were found to produce copious free radicals upon photoexcitation with UV-A and/or UV-B light, as determined by electron spin resonance spectroscopy. Among the sulfenamides, the most potent compounds were derived from dibenzazepine 7b and dihydroacridine 8b as determined in all of the four cancer cell lines.

摘要

合成了基于含S-N键化合物(亚磺酰胺)的新型1型光疗剂,评估了其自由基生成情况,并在四种癌细胞系(U937、HTC11、KB和HT29)中进行了体外细胞死亡疗效评估。通过电子自旋共振光谱测定,发现所有化合物在紫外-A和/或紫外-B光激发下都会产生大量自由基。在所有四种癌细胞系中测定发现,在亚磺酰胺中,最有效的化合物衍生自二苯并氮杂卓7b和二氢吖啶8b。

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